Enantiomers of 2′-fluoralkyl-6-nitroquipazine as serotonin transporter positron emission tomography imaging agents and antidepressant therapeutics
US7812162B2 · kind B2 · utility
Assignee
Inventors
Key dates
| Filing date | Apr 26, 2007 |
| Grant date | Oct 12, 2010 |
| Priority date | — |
| Expiry date | Sep 9, 2028 |
Classification
- Technology area (CPC A)Human Necessities
- CPC primaryA61P25/24
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Racemic mixtures and individual enantiomers of fluorine-18 or carbon-11 radio-labelled 2′-alkyl-6-nitroquipazine ligands are serotonin transporter (SERT) tracers for positron emission tomography (PET) imaging. The non-radioactive ligand forms possess therapeutic antidepressant in vitro and in vivo pharmacological binding profiles in rodent brain and cells expressing human serotonin transporter (hSERT). Twelve 2′-alkyl-6-nitroquipazine ligands potently bind in sub-nanomolar concentrations to the pre-synaptic SERT binding site where established antidepressant drugs bind and inhibit the re-uptake of the neurotransmitter serotonin (5-HT). In vivo tracer studies in rats as well as monkey PET scan trial have demonstrated the fluorine-18 and carbon-11 positron radionuclide labeled tracers perform as quantitative tracers of specific binding the SERT protein in live brain.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.